A method for isolating cytisine from plant material includes dissolving the plant material in an alcohol to form a liquid mixture, acidifying the liquid mixture by addition of a mineral acid, and concentrating the liquid mixture to form a concentrated aqueous solution. The method also includes extracting the concentrated aqueous solution with a first extractant to form a purified aqueous concentrate, alkalizing the purified aqueous concentrate with an alkaloid to form an alkaline aqueous concentrate, and extracting the alkaline aqueous concentrate with a second extractant. The method further includes removing the second extractant to obtain cytisine.

A method for isolating cytisine from plant material includes dissolving the plant material in an alcohol to form a liquid mixture, acidifying the liquid mixture by addition of a mineral acid, and concentrating the liquid mixture to form a concentrated aqueous solution. The method also includes extracting the concentrated aqueous solution with a first extractant to form a purified aqueous concentrate, alkalizing the purified aqueous concentrate with an alkaloid to form an alkaline aqueous concentrate, and extracting the alkaline aqueous concentrate with a second extractant. The method further includes removing the second extractant to obtain cytisine.

The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, O, or S; Y1 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 2 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y3 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 4 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y5 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); a and P are each present or absent and when present each is a bond.

The present invention relates to a macrocyclic JAK inhibitor and the use thereof. The present invention specifically relates to a compound as shown in formula I, or a stereoisomer or optical isomer thereof, a pharmaceutically acceptable salt thereof, and a prodrug or solvate thereof, and also relates to a pharmaceutical composition of the compound and the medical use thereof as a JAK inhibitor, and in the preparation of medicaments for preventing and/or treating diseases related to JAK, especially JAK1.

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The present invention relates to a macrocyclic JAK inhibitor and the use thereof. The present invention specifically relates to a compound as shown in formula I, or a stereoisomer or optical isomer thereof, a pharmaceutically acceptable salt thereof, and a prodrug or solvate thereof, and also relates to a pharmaceutical composition of the compound and the medical use thereof as a JAK inhibitor, and in the preparation of medicaments for preventing and/or treating diseases related to JAK, especially JAK1.

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A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.

Disclosed are novel analogs of cytisine, a process for their preparation, pharmaceutical compositions containing them, and their use in the prevention of or treatment of CNS disorders including addictive disorders.

Disclosed are novel analogs of cytisine, a process for their preparation, pharmaceutical compositions containing them, and their use in the prevention of or treatment of CNS disorders including addictive disorders.

The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.